异长春花苷内酰胺经酸催化形成喜果苷的研究(英文)  

Transformation of strictosamide to vincoside lactam by acid catalysis

作　　者：孟兆青[1,2,3] 刘文君[1,2] 李赞[3] 林蕴薇[3] 李孟璇[1,2] 安士影[1,2] 丁岗[1,2] 王振中[2] 萧伟[1,2] 徐进宜[3] 

机构地区：[1]江苏中康药物科技有限公司,南京210009 [2]中药制药过程新技术国家重点实验室,连云港222001 [3]中国药科大学,南京210009

出　　处：《中国天然药物》2013年第2期188-192,共5页

基　　金：supported by grants from "Eleventh Five-Year"major projects for innovation of new drug candidates(Nos.2009ZX09013-379,2012ZX09102201-017)~~

摘　　要：目的:鉴定异长春花苷内酰胺酸催化产物的结构,并探讨其反应机理。方法:用HPLC监控异长春花苷内酰胺酸催化反应过程,采用大孔吸附树脂纯化反应产物,以MS、NMR和ROESY分析确定产物结构。结果:异长春花苷内酰胺在酸催化条件下转化生成喜果苷,其转化率为52%。结论:异长春花苷内酰胺经酸催化可转化为喜果苷,其反应机理可能与化合物立体构型的稳定性有关,该发现提供了制备喜果苷的新方法。AIM： To identify the structure of the acid-catalyzed product of strictosamide and explore the reaction mechanism. METHODS： The acid-catalyzed reaction process of strictosamide was monitored by HPLC, and a macroporous resin was used to purify the reaction solution. The structure of the product was confirmed by MS, NMR, and ROESY spectra. RESULTS： The acid-catalyzed transformation yield from strictosamide to vincoside lactam was 52%. CONCLUSION： The reaction mechanism of the transformation from strictosamide to vincoside lactam may be related to the stability of the three-dimensional configuration of the compound. These results offer a new way to obtain vincoside lactam from the widely distributed indole alkaloid strictosamide by acid-catalysis.

关 键 词：异长春花苷内酰胺 喜果苷 酸催化 转化 

分 类 号：R284.2[医药卫生—中药学]